Isoxazoline parasiticide formulations

Inventors

Azamian, Bobak Robert • Ackermann, Douglas Michael • Hickok, Shawn D. • Vehige, Joseph G.

Assignees

Tarsus Pharmaceuticals Inc

Abstract

Disclosed herein are methods for treating or preventing ophthalmic and dermatologic conditions in a patient, including ocular surface conditions such as blepharitis. The methods can include topically administering directly to an ocular surface of one or more eyes of a patient in need of treatment thereof an effective amount of an isoxazoline parasiticide, formamidine parasiticide, or other active ingredient, formulated into an ophthalmic composition, the ophthalmic composition further comprising a pharmaceutically acceptable vehicle. Compositions are also disclosed.

Core Innovation

The invention relates to an ophthalmic composition for treating or preventing ophthalmic conditions that involve Demodex infestations. The composition includes an effective amount of an isoxazoline parasiticide for topical ocular administration, formulated in a sterile, non-irritating ophthalmic formulation for application to ocular surface structures.

The ophthalmic composition includes hydrogenated castor oil, a polysaccharide thickener, and glycerin. The isoxazoline parasiticide is present at about 0.10% to about 0.50% by weight, and the glycerin is present at about 0.5% to about 4% by weight, with respect to the total weight of the composition.

The document describes isoxazolines as GABA-chloride antagonists, leading to paralysis and death of Demodex mites. It also references preferential abdominal absorption versus ingestion and ex vivo observations of slowed Demodex mite movement, including abdomen and tail movement slowing, in connection with the proposed activity.

Representative isoxazoline parasiticides include fluralaner, sarolaner, lotilaner, afoxolaner, and fluxametamide. The document also describes optional additional antiparasitic actives, including formamidine parasiticides and phenylpyrazole parasiticides, and ophthalmic formulation elements such as solubilizers, tonicity agents, buffers, and preservatives, including optional exclusions such as essential oils.

Claims Coverage

The partial content includes one independent claim, directed to a defined ophthalmic composition with an isoxazoline parasiticide at a specified concentration range plus hydrogenated castor oil, a polysaccharide thickener, and glycerin within a specified range. Dependent claims refine additional composition elements and certain functional or scope limitations.

Across the independent claim, coverage is anchored on an ophthalmic composition containing an effective amount of an isoxazoline parasiticide at about 0.10% to about 0.50% by weight, together with hydrogenated castor oil, a polysaccharide thickener, and glycerin at about 0.5% to about 4% by weight.

Stated Advantages

Documented Applications